Assay Detail
Binding
CHEMBL863394
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Displacement of [3H]R-PIA from human adenosine A1 receptor transfected in CHO cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-uronamides as highly potent and selective agonists at the human A3 adenosine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 6.90 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL202189 | — | — | 1 | 8.70 |
| CHEMBL200705 | — | — | 1 | 8.49 |
| CHEMBL381868 | — | — | 1 | 8.34 |
| CHEMBL381408 | — | — | 1 | 7.86 |
| CHEMBL200184 | — | — | 1 | 7.43 |
| CHEMBL199877 | — | — | 1 | 7.32 |
| CHEMBL200072 | — | — | 1 | 7.12 |
| CHEMBL200099 | — | — | 1 | 7.12 |
| CHEMBL203357 | — | — | 1 | 7.05 |
| CHEMBL370446 | — | — | 1 | 7.04 |
| CHEMBL200407 | — | — | 1 | 6.90 |
| CHEMBL200854 | — | — | 1 | 6.84 |
| CHEMBL200732 | — | — | 1 | 6.71 |
| CHEMBL370187 | — | — | 1 | 6.29 |
| CHEMBL201427 | — | — | 1 | 6.20 |
| CHEMBL201706 | — | — | 1 | 5.88 |
| CHEMBL199414 | — | — | 1 | 5.77 |
| CHEMBL200279 | — | — | 1 | 5.76 |
| CHEMBL199541 | — | — | 1 | 5.70 |
| CHEMBL201324 | — | — | 1 | 5.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL202189 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL200705 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL381868 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL381408 | — | Ki | = | 13.9 | nM | 7.86 |
| CHEMBL200184 | — | Ki | = | 37.3 | nM | 7.43 |
| CHEMBL199877 | — | Ki | = | 47.8 | nM | 7.32 |
| CHEMBL200072 | — | Ki | = | 76.7 | nM | 7.12 |
| CHEMBL200099 | — | Ki | = | 75.8 | nM | 7.12 |
| CHEMBL203357 | — | Ki | = | 89.2 | nM | 7.05 |
| CHEMBL370446 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL200407 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL200854 | — | Ki | = | 144.0 | nM | 6.84 |
| CHEMBL200732 | — | Ki | = | 193.0 | nM | 6.71 |
| CHEMBL370187 | — | Ki | = | 507.0 | nM | 6.29 |
| CHEMBL201427 | — | Ki | = | 638.0 | nM | 6.20 |
| CHEMBL201706 | — | Ki | = | 1330.0 | nM | 5.88 |
| CHEMBL199414 | — | Ki | = | 1710.0 | nM | 5.77 |
| CHEMBL200279 | — | Ki | = | 1720.0 | nM | 5.76 |
| CHEMBL199541 | — | Ki | = | 1980.0 | nM | 5.70 |
| CHEMBL201324 | — | Ki | = | 4070.0 | nM | 5.39 |